Metabotropic glutamate receptors (mGluR)

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  1. GluR inhibitor

    (-)-Huperzine A is a naturally occurring sesquiterpene alkaloid compound found in the firmoss Huperzia serrata.
  2. mGluR Agonist

    LY-404039 is a drug used in scientific research that acts as a selective agonist for the metabotropic glutamate receptor group II subtypes mGluR2 and mGluR3. It has anxiolytic and antipsychotic effects in animal studies, but without causing sedation. Early human trials using a prodrug form of LY-404,039 called LY-214,0023 have also given encouraging results.
  3. mGluR5 modulator

    ADX-47273 is a drug used in scientific research which acts as a positive allosteric modulator selective for the metabotropic glutamate receptor subtype mGluR5.

  4. mGluR-2 antagonist

    LY 341495 has been shown to be a highly potent and selective group II metabotropic glutamate receptor (mGluR-2) antagonist with Ki / IC50 values are 2.3, 1.3, 173, 990, 6800, 8200 and 22000 nM for human mGluR-2, mGluR-3, mGluR-8 , mGluR-7a, mGluR-1a, mGluR-5a and mGluR-4a.
  5. mGluR5 PAM

    VU 0357121 is a positive allosteric modulator (PAM) of the metabotropic glutamate receptor 5 (mGlu5) with EC50 = 33 nM, 92% Glumax.
  6. CTEP is a highly potent, selective and orally bioavailable allosteric antagonist of mGlu5 receptor with an IC50 of 2.2 nM.
  7. mGlu4 receptor modulator

    Lu AF21934 is a selective and brain-penetrant mGlu4 receptor positive allosteric modulator with an IC50 of 500 nM for human mGlu4.
  8. mGluR5 positive allosteric modulator

    BMT-145027 is an mGluR5 positive allosteric modulator without inherent agonist activity, exhibits an EC50 of 47 nM.
  9. mGlu4 receptors modulator

    VU 0361737 is a selective positive allosteric modulator at mGluR-4 (EC50 values are 240 and 110 nM at human and rat receptors respectively).
  10. mGlu5 receptor antagonist

    MPEP is a potent and highly selective non-competitive antagonist at the mGlu5 receptor subtype (IC50 = 36 nM) and a positive allosteric modulator at mGlu4 receptors.
  11. GluR modulator

    VU 0364439 is a positive allosteric modulator (PAM) of mGlu4 receptors (EC50 = 19.8 nM in vitro for human mGlu4).
  12. mGluR antagonist

    SIB 1757 is a highly selective antagonist for the mGlu5 metabotropic glutamate receptor subtype.
  13. mGluR antagonist

    SIB 1893 is a highly selective non-competitive antagonist for the metabotropic glutamate mGlu5 receptor subtype.
  14. mGluR1 modulator

    CPPHA is a selective positive allosteric modulator of mGluR5 receptor.
  15. mGlu5 antagonist

    MTEP hydrochloride is a potent, selective and non-competitive mGlu5 antagonist with IC50 and Ki of 5 nM and 16 nM, respectively.
  16. Noopept is a medication promoted and prescribed in Russia and neighbouring countries as a nootropic.
  17. mGluR1 antagonist

    DL-AP3, a racemic preparation of D-AP3 and L-AP3, is an inhibitor of phosphoserine phosphatase and an antagonist of the metabotropic glutamate receptor (mGluR), blocking phosphoinositide turnover mediated by the mGluR.
  18. glutamate receptors agonist

    (S)-Glutamic acid acts as an excitatory transmitter and an agonist at all subtypes of glutamate receptors (metabotropic, kainate, NMDA, and AMPA).
  19. mGluR agonist

    (S)-3,5-DHPG is an agonist of the group I metabotropic glutamate receptors (mGluRs), binding both mGluR1a and mGluR5a (Ki = 0.9 and 3.9 uM, respectively) but not ionotropic glutamate receptors.
  20. mGluR5 antagonist

    AZD 9272 is a brain penetrant mGluR5 antagonist.
  21. mGlu1 receptor modulator

    FITM is a negative allosteric modulator of mGlu1 receptor with a Ki of 2.5 nM.
  22. mGluR5 antagonist

    Fenobam is a selective, orally active, and non-competitive mGluR5 antagonist acting at an allosteric modulatory site (Kd values are 54 and 31 nM for rat and human recombinant mGlu5 receptors, respectively).
  23. mGlu1 receptor antagonist

    JNJ16259685 is a selective antagonist of mGlu1 receptor, and inhibits the synaptic activation of mGlu1 in a concentration-dependent manner with IC50 of 19 nM.
  24. group I/group II mGluR antagonist

    (S)-MCPG is the active isomer of (RS)-MCPG, non-selective group I/group II metabotropic glutamate receptor antagonist.

  25. mGlu1 receptors modulator

    Ro 67-7476 is a positive allosteric modulator of mGlu1 receptors.
  26. mGluR 1 allosteric antagonist

    CFMTI is a potent and selective metabotropic glutamate receptor (mGluR) 1 allosteric antagonist with IC50 of 2.6 nM.
  27. metabotropic receptor agonist

    trans-ACPD, a metabotropic receptor agonist, produces calcium mobilization and an inward current in cultured cerebellar Purkinje neurons.
  28. group I/group II mGluR antagonist

    E4CPG is a novel group I/group II metabotropic glutamate receptor antagonist, more potent than (RS)-MCPG .
  29. group I/group II mGluR antagonist

    (RS)-MCPG is a non-selective group I/group II metabotropic glutamate receptor antagonist.
  30. group II (mGlu2/3) receptor agonist

    Eglumegad (LY354740) is a highly potent and selective group II (mGlu2/3) receptor agonist with IC50s of 5 and 24 nM on transfected human mGlu2 and mGlu3 receptors, respectively.
  31. group III mGluR receptors agonist

    O-Phospho-L-serine is the immediate precursor to L-serine in the serine synthesis pathway, and an agonist at the group III mGluR receptors (mGluR4, mGluR6, mGluR7, and mGluR8); O-Phospho-L-serine also acts as a weak antagonist for mGluR1 and a potent antagonist for mGluR2.
  32. mGlu4 receptor modulator

    TCN238 is a positive allosteric mGlu4 receptor modulator with an EC50 of 1 μM.
  33. mGluRs M3 agonist

    L-APB is a potent and specific agonist for the group III mGluRs, with EC50s of 0.13, 0.29, 1.0, 249 μM for mGlu4, mGlu8, mGlu6 and mGlu7 receptors, respectively.
  34. mGlu5 receptor antagonist

    Methoxy-PEPy is a potent and highly selective mGlu5 receptor antagonist with IC50 of 1 nM.
  35. partial mGluR4 agonist

    (1R,2S)-VU0155041, Cis regioisomer of VU0155041, is a partial mGluR4 agonist with an EC50 of 2.35 μM.
  36. mGlu5 PAM

    ML-254, also known as VU0430644; is Positive Allosteric Modulators (PAMs) of mGlu5 with Competitive MPEP-Site Interaction.
  37. mGlu1 receptor agonist

    Ro0711401 is a mGlu1 receptor agonist.
  38. mGluR II agonist

    Xanthurenic acid is a putative endogenous Group II metabotropic glutamate receptor agonist, on sensory transmission in the thalamus.
  39. mGluR1b antagonist

    CPCCOEt is a low affinity, selective, non-competitive antagonist of the metabotropic glutamate receptor subtype mGluR1b.
  40. mGlu1 receptorsant agonist

    YM 298198 Hydrochloride is a non-competitive antagonist with high affinity and selectivity for mGlu1 receptors (Ki = 19 nM).
  41. PAM of mGluR4

    VU0155041 is a potent, selective positive allosteric modulator (PAM) of mGluR4, with EC50s of 798 nM and 693 nM for human and rat mGluR4, respectively. VU0155041 has potential for the research of Parkinson's disease (PD).

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